Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 544/400)
-
Patent number: 7199158Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 18, 2005Date of Patent: April 3, 2007Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
-
Patent number: 7160887Abstract: Compounds of a formula: wherein Ring A represents an optionally-substituted aromatic ring; Ring B represents an optionally-substituted cyclic hydrocarbon group; Z represents an optionally-substituted cyclic group; R1 represents a hydrogen atom, an optionally-substituted hydrocarbon group, an optionally-substituted heterocyclic group, or an acyl group; R2 represents an optionally-substituted amino group; D represents a chemical bond or a divalent group; E represents —CO—, —CON(Ra)—, COO—, N(Ra)CON(Rb)—, —N(Ra)COO—, —N(Ra)SO2—, N(Ra)—, —O—, —S—, —SO— or —SO2— (in which Ra and Rb each independently represent a hydrogen atom or an optionally-substituted hydrocarbon group); G represents a chemical bond or a divalent group; L represents (1) a chemical bond or (2) a divalent hydrocarbon group optionally having from 1 to 5 substituents selected from; (i) a C1-6 alkyl group, (ii) a halogeno-C1-6 alkyl group, (iii) a phenyl group, (iv) a benzyl group, (v) an optionally-substituted amino group, (vi) an optionallyType: GrantFiled: October 19, 1999Date of Patent: January 9, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Satoru Oi, Nobuhiro Suzuki, Kazuyoshi Aso, Yoshihiro Banno
-
Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
-
Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
-
Patent number: 7074820Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 23, 2001Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventor: Thomas Antonsson
-
Patent number: 7030122Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin receptors and dopamine receptors. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, and senile dementia.Type: GrantFiled: March 27, 2003Date of Patent: April 18, 2006Assignee: Sepracor Inc.Inventors: James R. Hauske, Joanne M. Holland, Heike S. Radeke
-
Patent number: 7026323Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: September 22, 2004Date of Patent: April 11, 2006Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
-
Patent number: 6995269Abstract: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: March 4, 2003Date of Patent: February 7, 2006Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, David Duhl
-
Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
-
Patent number: 6964963Abstract: The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl group is cleaved off, and further describes 4-acetamino-1-naphthol ethers obtained thereby.Type: GrantFiled: August 27, 2002Date of Patent: November 15, 2005Assignee: Bayer AktiengesellschaftInventors: Joachim Komoschinski, Herbert Diehl
-
Patent number: 6960588Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.Type: GrantFiled: September 12, 2000Date of Patent: November 1, 2005Assignee: Altana Pharma AGInventor: Thomas Martin
-
Patent number: 6906073Abstract: The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 29, 2002Date of Patent: June 14, 2005Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
-
Patent number: 6887876Abstract: Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: GrantFiled: December 11, 2001Date of Patent: May 3, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ellen W. Baxter, Samuel O. Nortey, Allen B. Reitz
-
Patent number: 6887903Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.Type: GrantFiled: October 14, 1999Date of Patent: May 3, 2005Assignee: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
-
Patent number: 6878707Abstract: Compounds of formula (I) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmaceutically acceptable salts thereof; and enantiType: GrantFiled: January 16, 2001Date of Patent: April 12, 2005Assignee: Novartis AGInventor: Gary Michael Ksander
-
Patent number: 6852723Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 11, 2003Date of Patent: February 8, 2005Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn, Tim Marquart, Prabha N. Ibrahim, Venkata P. Palle
-
Patent number: 6846824Abstract: Compounds of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.Type: GrantFiled: March 23, 2001Date of Patent: January 25, 2005Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Channaveerappa Bajji, Shivaramayya Kalchar, Rajagopalan Ramanujam, Ranjan Chakrabarti, Javed Iqbal, Ranga Madhavan Gurram
-
Patent number: 6844299Abstract: This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier such as diacid or cyclic anhydride and a polyamine. The hydrocarbon acid makes up the non-polar hydrocarbon portion of the dispersant and the polyamine functions as the polar headgroup. The diacid or cyclic anhydride provides a means for attaching the polar polyamine to the dispersant structure through an amide linkage. Different dispersant structures are obtained by varying the hydrocarbon acid, the polyol and the nature of the polyamine.Type: GrantFiled: February 20, 2003Date of Patent: January 18, 2005Assignee: BP Corporation North America Inc.Inventors: Paul W. Bessonette, Patrick E. Godici, Kim E. Fyfe, Jeenok T. Kim
-
Patent number: 6838460Abstract: The present invention relates to phenylamidines of general formula wherein R6 and R7 are defined as in claim 1, the tautomers, the stereoisomers including mixtures thereof and the salts thereof, particularly their physiologically acceptable salts with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably antithrombotic effects, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: January 13, 2001Date of Patent: January 4, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Brian Guth
-
Publication number: 20040158062Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds are useful in the treatment of benign prostatic hyperplasia.Type: ApplicationFiled: February 9, 2004Publication date: August 12, 2004Applicant: Pfizer IncInventors: Jens Bertil Ahman, Paul Blaise Hodgson, Sarah Jane Lewandowski, Robert Walton
-
Patent number: 6770649Abstract: Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, wherein R6, R7, A and Z have the meanings given in the description, and pharmaceutical compositions containing these compounds, as well as a process for the preparation of such compounds and intermediate products of this process.Type: GrantFiled: September 13, 2002Date of Patent: August 3, 2004Assignee: Solvay Pharmaceuticals GmbHInventors: Daniel Jasserand, Ulf Preuschoff, Jochen Antel, Samuel David, Holger Sann, Reinhard Brueckner, Dania Reiche, Christian Eeckhout
-
Patent number: 6753327Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.Type: GrantFiled: October 11, 2000Date of Patent: June 22, 2004Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
-
Publication number: 20040116693Abstract: The present invention relates to a process for effectively preparing prostaglandin derivatives and to a stereospecific alkyl halide containing 15S-alcohol group as a starting material.Type: ApplicationFiled: October 24, 2003Publication date: June 17, 2004Inventors: Won-Hun Ham, Chang-Young Oh, Kee-Young Lee, Yong-Hyun Kim, Yiu-Suk Lee
-
Patent number: 6747027Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: June 8, 2004Assignee: Pharmacia CorporationInventors: Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
-
Publication number: 20040058932Abstract: A compound of the formula 1Type: ApplicationFiled: September 10, 2003Publication date: March 25, 2004Applicant: Pfizer Inc.Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Molly A. McGlynn, Christopher S. Poss
-
Publication number: 20040054172Abstract: The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystaline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: June 19, 2003Publication date: March 18, 2004Inventors: Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael Huai Gu Chen, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
-
Publication number: 20040038983Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin receptors and dopamine receptors. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, and senile dementia.Type: ApplicationFiled: March 27, 2003Publication date: February 26, 2004Inventors: James R. Hauske, Joanne M. Holland, Heike S. Radeke
-
Patent number: 6686360Abstract: The present invention relates to a compound selected from those of formula (I): wherein: R1 represents alkyl, R2 represents hydroxy, alkoxy, or amino, n represents an integer from 1 to 12 inclusive, R3 represents: hydrogen, optionally substituted alkyl, cycloalkyl, pyrimidinyl or optionally substituted phenyl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the prevention or treatment of acute and chronic cell ischaemia.Type: GrantFiled: July 16, 2002Date of Patent: February 3, 2004Assignee: Les Laboratoires ServierInventors: Serge Labidalle, Jean-Paul Tillement, Bernard Testa, Roméo Cecchelli, Alain Le Ridant, Catherine Harpey, Michael Spedding, Esther Schenker
-
Patent number: 6677336Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: January 13, 2004Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Grigory Nudelman, Tim Marquart, Brent K. Blackburn, Venkata P. Palle
-
Publication number: 20030232742Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug is chemically stable under physiological conditions and can be used for the manufacture of physically stable aqueous formulations. It has a cleavage site which is recognised by FAP&agr;, and the drug released by the enzymatic activity of FAP&agr; is cytotoxic or cytostatic under physiological conditions.Type: ApplicationFiled: November 9, 2001Publication date: December 18, 2003Inventors: Stefan Peters, Dietmar Leipert, Christian Eickmeier, John Edward Park, Martin Lenter, Pilar Garin-Chesa, Juergen Mack
-
Publication number: 20030228986Abstract: This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier such as diacid or cyclic anhydride and a polyamine. The hydrocarbon acid makes up the non-polar hydrocarbon portion of the dispersant and the polyamine functions as the polar headgroup. The diacid or cyclic anhydride provides a means for attaching the polar polyamine to the dispersant structure through an amide linkage. Different dispersant structures are obtained by varying the hydrocarbon acid, the polyol and the nature of the polyamine.Type: ApplicationFiled: February 20, 2003Publication date: December 11, 2003Inventors: Paul W. Bessonette, Patrick E. Godici, Kim E. Fyfe, Jeenok T. Kim
-
Publication number: 20030220344Abstract: Methods are provided for treating arrhythmias including tachycardias, such as idiopathic ventricular tachycardia, ventricular fibrillation, and Torsade de Pointes (TdP) in a manner that minimizes undesirable side effects.Type: ApplicationFiled: April 3, 2003Publication date: November 27, 2003Inventors: Luiz Belardinelli, Charles Antzelevitch, Brent Blackburn
-
Publication number: 20030212056Abstract: The present application describes novel &bgr;-sulfone derivatives of formula I: 1Type: ApplicationFiled: November 1, 2002Publication date: November 13, 2003Inventors: Jingwu Duan, Gregory R. Ott
-
Publication number: 20030208068Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.Type: ApplicationFiled: March 13, 2003Publication date: November 6, 2003Inventors: Jiacheng Zhou, Lynette May Oh, Philip Ma
-
Patent number: 6638927Abstract: Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: August 31, 2001Date of Patent: October 28, 2003Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, Zhi-Jie Ni, David Duhl, Effie Tozzo, Kirk Johnson, David C. Myles
-
Publication number: 20030199698Abstract: Novel compounds of the formula I 1Type: ApplicationFiled: May 16, 2003Publication date: October 23, 2003Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
-
Patent number: 6635621Abstract: This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.Type: GrantFiled: January 30, 2002Date of Patent: October 21, 2003Assignee: Naeja Pharmaceutical Inc.Inventors: Rajeshwar Singh, Nian Zhou, Andhe V. N. Reddy, George Thomas, Qizhu Ding, Jadwiga Kaleta, Ronald George Micetich, Mark Whittaker
-
Publication number: 20030181442Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: November 27, 2001Publication date: September 25, 2003Applicant: BAYER CORPORATIONInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
-
Publication number: 20030171579Abstract: The invention relates to novel compounds of formula (I), wherein R, R1 and R2 have the meaning as cited claim 1. According to the invention, the compounds are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis post-angioplasty, intermittent claudication, tumours, tumour related illnesses and/or tumour metastases.Type: ApplicationFiled: January 27, 2003Publication date: September 11, 2003Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
-
Publication number: 20030144277Abstract: The present application describes modulators of CCR3 of formula (I): 1Type: ApplicationFiled: September 18, 2002Publication date: July 31, 2003Inventor: George V. DeLucca
-
Publication number: 20030125281Abstract: Described is a deliverable composition with low toxicity comprising an amphipathic compound, a polycation, and a siRNA. The composition may be used in the process of delivering a siRNA to an animal cell or more particularly, a mammal cell.Type: ApplicationFiled: May 28, 2002Publication date: July 3, 2003Inventors: David Lewis, James E. Hagstrom, Hans Herweijer, Aaron G. Loomis, Sean D. Monahan, Jon A. Wolff
-
Patent number: 6586187Abstract: Compounds of the formula are useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula I are also provided.Type: GrantFiled: April 13, 2000Date of Patent: July 1, 2003Assignee: WyethInventors: Ariamala Gopalsamy, Hui Y. Yang
-
Publication number: 20030105097Abstract: The invention provides compounds of formula (I) 1Type: ApplicationFiled: May 6, 2002Publication date: June 5, 2003Applicant: Pfizer Inc.Inventors: Andrew Simon, Alan Stobie
-
Publication number: 20030105132Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: ApplicationFiled: March 12, 2002Publication date: June 5, 2003Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
-
Publication number: 20030096824Abstract: The present invention relates to phenylamidines of general formula 1Type: ApplicationFiled: October 21, 2002Publication date: May 22, 2003Inventors: Frank Himmelsbach, Brian Guth
-
Patent number: 6562825Abstract: The invention provides compounds of general formula (I) wherein R1, R2, R3, R4, R5, X, Y, Z, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.Type: GrantFiled: August 17, 2000Date of Patent: May 13, 2003Assignee: Astrazeneca UK LimitedInventors: Andrew J G Baxter, Stephen J Brough, Nicholas D Kindon, Thomas McInally, Bryan Roberts
-
Patent number: 6555541Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: July 10, 2000Date of Patent: April 29, 2003Assignee: Astrazeneca UK LimitedInventors: Mark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
-
Patent number: 6552023Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: April 22, 2003Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn, Tim Marquart, Prabha N. Ibrahim, Venkata P. Palle
-
Patent number: 6534499Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: March 18, 2003Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
-
Patent number: RE39088Abstract: An amide compound of the formula (I): ? wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-?, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.Type: GrantFiled: August 15, 1996Date of Patent: May 2, 2006Assignee: Japan Tobacco, Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe